α-CGRP   Click here for help

GtoPdb Ligand ID: 681

Synonyms: α-calcitonin gene-related peptide (αCGRP, human) | calcitonin gene-related peptide 1 (CGRP)
Compound class: Endogenous peptide in human, mouse or rat
Comment: This peptide is an isoform of calcitonin, encoded by the same gene and produced by alternative splicing. Please note that each peptide is represented by a different UniProt ID.
Species: Human
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Ligand Activity Visualisation Charts

These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.

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View interactive charts of activity data across species

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View more information in the IUPHAR Pharmacology Education Project: α-cgrp

Natural/Endogenous Targets
Target
AM1 receptor
AM2 receptor
AMY1 receptor
AMY2 receptor
AMY3 receptor
CGRP receptor
CT receptor
Selectivity at GPCRs
Key to terms and symbols Click column headers to sort
Target Sp. Type Action Value Parameter Concentration range (M) Reference
AM1 receptor Ligand is endogenous in the given species Hs Agonist Full agonist 6.0 pKd - 9
⤷ pKd 6.0 [9]
CGRP receptor Ligand is endogenous in the given species Hs Agonist Full agonist 9.7 – 10.0 pKi - 1,9
⤷ pKi 9.7 – 10.0 [1,9]
AM2 receptor Ligand is endogenous in the given species Hs Agonist Full agonist 6.5 – 6.8 pKi - 1,3
⤷ pKi 6.5 – 6.8 [1,3]
AMY1 receptor Ligand is endogenous in the given species Hs Agonist Full agonist 8.7 – 10.8 pEC50 - 5-8,10
⤷ pEC50 8.7 – 10.8 [5-8,10]
AMY3 receptor Ligand is endogenous in the given species Hs Agonist Full agonist 7.6 – 9.7 pEC50 - 5-7
⤷ pEC50 7.6 – 9.7 [5-7]
AMY2 receptor Ligand is endogenous in the given species Hs Agonist Full agonist 6.2 – 9.7 pEC50 - 5-7
⤷ pEC50 6.2 – 9.7 [5-7]
CT receptor Ligand is endogenous in the given species Hs Agonist Full agonist 6.2 – 8.4 pEC50 - 5-6,8,12
⤷ pEC50 6.2 – 8.4 [5-6,8,12]
Additional information and targets (data relate to human unless otherwise stated)
Description Data Reference
Potency order of endogenous ligands at CT receptor calcitonin (CALCA, P01258) ≥ amylin (IAPP, P10997), α-CGRP (CALCA, P06881), β-CGRP (CALCB, P10092) > adrenomedullin (ADM, P35318), adrenomedullin 2/intermedin (ADM2, Q7Z4H4)
Potency order of endogenous ligands at AMY1 receptor amylin (IAPP, P10997) ≥ α-CGRP (CALCA, P06881), β-CGRP (CALCB, P10092) > adrenomedullin 2/intermedin (ADM2, Q7Z4H4) ≥ calcitonin (CALCA, P01258) > adrenomedullin (ADM, P35318)
Potency order of endogenous ligands at CGRP receptor α-CGRP (CALCA, P06881), β-CGRP (CALCB, P10092) > adrenomedullin (ADM, P35318) ≥ adrenomedullin 2/intermedin (ADM2, Q7Z4H4) > amylin (IAPP, P10997)
Potency order of endogenous ligands at AM1 receptor adrenomedullin (ADM, P35318) > adrenomedullin 2/intermedin (ADM2, Q7Z4H4) > α-CGRP (CALCA, P06881), β-CGRP (CALCB, P10092), amylin (IAPP, P10997)
Potency order of endogenous ligands at AM2 receptor adrenomedullin (ADM, P35318) ≥ adrenomedullin 2/intermedin (ADM2, Q7Z4H4) ≥ α-CGRP (CALCA, P06881), β-CGRP (CALCB, P10092) > amylin (IAPP, P10997)
Potency order of endogenous ligands at AMY3 receptor amylin (IAPP, P10997) > α-CGRP (CALCA, P06881), β-CGRP (CALCB, P10092) ≥ adrenomedullin 2/intermedin (ADM2, Q7Z4H4) ≥ calcitonin (CALCA, P01258) > adrenomedullin (ADM, P35318)
Other ligands which bind to or alter the activity of this ligand
Key to terms and symbols Click column headers to sort
Ligand Sp. Type Action Value Parameter Concentration range (M) Reference
fremanezumab Peptide Approved drug Primary target of this compound Hs Antibody Binding >10.3 pKd - 11
⤷ pKd >10.3 (Kd <5x10-11 M) [11]
galcanezumab Peptide Approved drug Primary target of this compound Hs Antibody Binding 8.7 pKd - 2
⤷ pKd 8.7 (Kd 2.2x10-9 M) [2]
eptinezumab Peptide Approved drug Primary target of this compound Hs Antibody Binding 10.0 pEC50 - 4
⤷ pEC50 10.0 (EC50 1.03x10-10 M) [4]
Description: Binding affinity for α-CGRP determined in an ELISA.
Ligand mentioned in the following text fields
Calcitonin receptors overview